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在Sarpagine和Macroline类化合物的集体合成中,采用类化合物的灵感

Hikaru Aoyama¹, Caitlin Davies¹, Jie Liu¹

¹Max Planck Institute of Molecular Physiology, Department of Chemical Biology, 44227, Dortmund, Germany.

Chemistry (Weinheim an der Bergstrasse, Germany)

|September 27, 2023

概括

这项研究开发了一种新方法,以创建各种印类化物启发的化合物. 一些伪天然产品有效调节蛋白,抑制细胞分裂.

科学领域:

药用化学医学化学
化学生物学化学生物学

背景情况:

有效地访问类似自然产品的化学空间对于发现生物相关化合物至关重要.
印度醇化物代表着丰富的生物活性分子来源,但它们复杂的结构带来了合成挑战.

研究的目的:

开发一种不同的合成策略,以产生一种因多尔类化合物启发的化合物库.
探索两个不同的分子设计原则:以生物学为导向的合成和伪自然产品.
识别具有新生物活性的化合物,特别是影响细胞分裂的化合物.

主要方法:

采用了不同的合成中间策略.
利用酸催化和锡介导条件进行选择性内分子化 (C-或N-).
在四个类别中生成了84个化合物的库.
通过细胞涂漆试验和亚型分析进行了形态分析.

主要成果:

合成产生了84种来自四个不同的类别的印类类激发化合物.
来自不同设计原则的化合物表现出不同的生物活性概况.
亚概况分析表明,伪天然产品被丰富在氨酸调节剂中.
鉴定出了抑制体外管聚合和线性进展的特定化合物.

结论:

一种不同的合成方法有效地产生了一种多样化的印类化物启发的图书馆.
这项研究成功地将分子设计原则与不同的生物活动概况联系起来.
伪天然产品衍生品通过向氨酸,显示出作为抗真菌剂的前景.

关键词:

以生物学为导向的合成.不同的合成分离.形态分析形态分析伪天然产品是假天然产品.素聚合抑制剂素聚合抑制剂

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